6-methylamino-3,7-dihydro-purin-2-one | 24391-35-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 英文名称: 6-methylamino-3,7-dihydro-purin-2-one
• 英文别名: 6-Methylamino-3,7-dihydro-purin-2-on；2-Hydroxy-6-methylaminopurine；6-(methylamino)-3,7-dihydropurin-2-one
• CAS: 24391-35-3
• 化学式: C₆H₇N₅O
• 分子量: 165.154
• InChiKey: LPQHPQFWXGHHAI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  82.2
• 氢给体数：
  3
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  6-硫代-2-羟基嘌呤 在 sodium hydroxide 、 乙醇 作用下， 生成 6-methylamino-3,7-dihydro-purin-2-one
  参考文献：
  名称：

  Synthesis of Potential Anticancer Agents. XIX. 2-Substituted N⁶-Alkyladenines

  摘要：

  DOI：

  10.1021/ja01524a037

文献信息

• NOVEL KINASE MODULATORS
  申请人：MUTHUPPALANIAPPAN Meyyappan

  公开号：US20110118257A1

  公开（公告）日：2011-05-19

  The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

  本发明提供了PI3K蛋白激酶调节剂，其制备方法，含有它们的药物组合物，以及使用它们进行激酶介导的疾病或紊乱的治疗、预防和/或改善的方法。
• Method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK)
  申请人：CHEN Han-Min

  公开号：US20140303112A1

  公开（公告）日：2014-10-09

  The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.

  本发明涉及一种治疗疾病或病情的方法，该疾病或病情容易通过AMPK激活剂和公式化合物得到改善，这些化合物有助于激活AMP激活蛋白激酶（AMPK），并将这些化合物用于预防或治疗疾病，包括糖尿病前期、2型糖尿病、X综合症、代谢综合征和肥胖症。
• NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
  申请人：NAGARATHNAM Dhanapalan

  公开号：US20120289496A1

  公开（公告）日：2012-11-15

  The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

  本发明提供了PI3K蛋白激酶调节剂，其制备方法，含有它们的药物组合物，以及使用它们进行治疗、预防和/或改善激酶介导的疾病或紊乱的方法。
• Purines. LV. Syntheses and Cytokinin Activities of Some Adenine and Adenosine Derivatives Related to 1'-Methylzeatin.
  作者：Tozo FUJII、Masashi OHBA、Hitoshi KAWAMURA、Tsuyoshi HANEISHI、Satoshi MATSUBARA

  DOI：10.1248/cpb.41.1362

  日期：——

  (1'S)-1-Methyl-cis-zeatin [(1'S)-2] and its 9-β-D-ribofuranoside [(1"S)-4] were synthesized from L-alanine through [S-(Z)]-4-amino-2-methyl-2-penten-1-ol ethanedioate [(S)-3]. Condensations of 2-hydroxy-6-methylthiopurine (16) with the trans-isomeric amine salt [(S)-15], its enantiomer [(R)-15], and the racemic modification [(±)-15] furnished (1'S)-, (1'R)-, and (±)-2-hydroxy-1'-methyl-trans-zeatine (6), respectively. A similar condensation of 16 with methylamine yielded 2-hydroxy-N6-methyladenine (7). These adenine derivatives were tested for cytokinin activity in the tobacco callus bioassay, and the order of their activity was (1'R)-6>(±)-6>(1'S)-2>7; on the other hand, (1"S)-4 and (1'S)-6 were completely inactive at 0.1-100μM and 0.01-10μM concentrations, respectively. As a result of the above syntheses of (1'R)-6, (1'S)-6, (±)-6, and 7, the gross structures of a marine green alga cytokinin and of a blue coral cytokinin were established to be 6 and 7, respectively.

  以L-丙氨酸为原料，通过[S-(Z)]合成(1'S)-1-甲基-顺式玉米素[(1'S)-2]及其9-β-D-呋喃核苷[(1"S)-4] -4-氨基-2-甲基-2-戊烯-1-醇乙二酸酯[(S)-3] 2-羟基-6-甲基硫嘌呤(16)与反式异构胺盐[(S)-15]、其对映体[(R)-15]和外消旋体[(±)-15]提供(1'S)-、(1'R)-和(± )-2-羟基-1'-甲基-反式-玉米丁(6)，分别用甲胺进行类似的缩合，得到2-羟基-N6-甲基腺嘌呤(7)。烟草愈伤组织生物测定中的细胞分裂素活性，其活性顺序为(1'R)-6>(±)-6>(1'S)-2>7；另一方面，(1"S)-4和(1'S)-6 分别在 0.1-100μM 和 0.01-10μM 浓度下完全失活。作为(1'R)-6、(1'S)-6、(±)-6和7的上述合成的结果，海洋绿藻细胞分裂素和蓝珊瑚细胞分裂素的总体结构被确定为分别为6和7。
• Compounds as modulators of protein kinases
  申请人：Rhizen Pharmaceuticals SA

  公开号：US10220035B2

  公开（公告）日：2019-03-05

  The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

  本发明提供了 PI3K 蛋白激酶调节剂、制备方法、含有这些调节剂的药物组合物以及用它们治疗、预防和/或改善激酶介导的疾病或紊乱的方法。